PMID- 17906643
OWN - NLM
STAT- MEDLINE
DCOM- 20071011
LR  - 20071001
IS  - 1474-1784 (Electronic)
IS  - 1474-1776 (Linking)
VI  - 6
IP  - 10
DP  - 2007 Oct
TI  - Design of selective nuclear receptor modulators: RAR and RXR as a case study.
PG  - 811-20
AB  - Retinoic acid receptors (RARs) and retinoid X receptors (RXRs) are members of the 
      nuclear receptor superfamily whose effects on cell growth and survival can be 
      modulated therapeutically by small-molecule ligands. Although compounds that 
      target these receptors are powerful anticancer drugs, their use is limited by 
      toxicity. An improved understanding of the structural biology of RXRs and RARs 
      and recent advances in the chemical synthesis of modified retinoid and rexinoid 
      ligands should enable the rational design of more selective agents that might 
      overcome such problems. Here, we review structural data for RXRs and RARs, 
      discuss strategies in the design of selective RXR and RAR modulators, and 
      consider lessons that can be learned for the design of selective nuclear-receptor 
      modulators in general.
FAU - de Lera, Angel R
AU  - de Lera AR
AD  - Universidade de Vigo, Departamento de Quimica Organica, Facultad de Quimica, 
      36310 Vigo, Spain.
FAU - Bourguet, William
AU  - Bourguet W
FAU - Altucci, Lucia
AU  - Altucci L
FAU - Gronemeyer, Hinrich
AU  - Gronemeyer H
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
PL  - England
TA  - Nat Rev Drug Discov
JT  - Nature reviews. Drug discovery
JID - 101124171
RN  - 0 (Ligands)
RN  - 0 (Receptors, Retinoic Acid)
RN  - 0 (Retinoid X Receptors)
RN  - 0 (Retinoids)
SB  - IM
MH  - Animals
MH  - *Drug Design
MH  - Humans
MH  - Ligands
MH  - Models, Molecular
MH  - Molecular Structure
MH  - Protein Binding
MH  - *Receptors, Retinoic Acid/agonists/antagonists & inhibitors/chemistry
MH  - Retinoid X Receptors/agonists/antagonists & inhibitors/chemistry
MH  - *Retinoids/chemical synthesis/chemistry/pharmacology
RF  - 59
EDAT- 2007/10/02 09:00
MHDA- 2007/10/12 09:00
CRDT- 2007/10/02 09:00
PHST- 2007/10/02 09:00 [pubmed]
PHST- 2007/10/12 09:00 [medline]
PHST- 2007/10/02 09:00 [entrez]
AID - nrd2398 [pii]
AID - 10.1038/nrd2398 [doi]
PST - ppublish
SO  - Nat Rev Drug Discov. 2007 Oct;6(10):811-20. doi: 10.1038/nrd2398.